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Abstract
5-Substituted-1H-tetrazoles (RCN4H) are often used as metabolism-resistant isosteric
replacements for carboxylic acids (RCO2H) in SAR-driven medicinal chemistry analogue
syntheses. This review provides a brief summary of the medicinal chemistry of tetrazolic
acids and highlights some examples of tetrazole-containing drug substances in the
current literature. A survey of representative literature procedures for the preparation
of 5-substituted-1H-tetrazoles, focusing on preparations from aryl and alkyl nitriles,
is presented in sections by generalized synthetic methods.